申请人:Merrell Dow Pharmaceuticals Inc.
公开号:US04595687A1
公开(公告)日:1986-06-17
Sparsomycin derivatives of the formula ##STR1## wherein X and Y are each independently an oxo or an imino group; n is 0 or the integer 1 or 2; R.sub.1 is a hydrogen or 1 to 4 carbon alkyl group; R.sub.2 is a hydrogen, a 1 to 4 carbon alkyl, a 2 to 5 carbon acyl or a benzoyl group; and R is a 1 to 6 carbon alkyl, 3 to 8 carbon alkenyl, cyanomethyl carboxymethyl, carbalkoxymethyl wherein the alkoxy moiety is a 1 to 4 carbon alkoxy group, nitromethyl, alkylcarbonylmethyl wherein the alkyl moiety is a 1 to 4 carbon alkyl group, pyridyl, furanyl, or furfuryl group or a phenyl or benzyl group optionally substituted by a methylenedioxy or one to two halogen, 1 to 4 carbon alkyl, 1 to 4 carbon alkoxy, 1 to 4 carbon alkylthio, hydroxy, nitro or cyano groups or a pharmaceutically acceptable acid addition salt thereof. Also described are their use as antiprotozoals and antibacterials.
该文描述了Sparsomycin衍生物的结构式,其中X和Y分别独立地为氧代或亚氨基基团;n为0或整数1或2;R1为氢或1至4个碳原子的烷基基团;R2为氢、1至4个碳原子的烷基、2至5个碳原子的酰基或苯甲酰基基团;R为1至6个碳原子的烷基、3至8个碳原子的烯基、氰甲基羧甲基、羧基烷氧甲基(其中烷氧基是1至4个碳原子的烷氧基团)、硝基甲基、烷基羰基甲基(其中烷基是1至4个碳原子的烷基团)、吡啶基、呋喃基或呋喃甲基基团或苯基或苄基基团(可选地被一个亚甲二氧基或1至2个卤素、1至4个碳原子的烷基、1至4个碳原子的烷氧基、1至4个碳原子的烷硫基、羟基、硝基或氰基基团取代),或其药学上可接受的酸加合盐。还描述了它们作为抗原虫和抗菌剂的用途。